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Journal of the Korean Chemical Society (JKCS)

ISSN 1017-2548(Print)
ISSN 2234-8530(Online)
Volume 34, Number 5
JKCSEZ 34(5)
October 20, 1990 

Structure-Activity Relationship (Ⅰ). Conformational Analysis of 3-Phenyl-5,5-dimethyloxazolidine-2,4-diones and their Antifungal Activities

구조-활성 관계 (제 1 보). 3-Phenyl-5,5-dimethyloxazolidine-2,4-diones 와 그들의 Antifungal Activity 에 관한 형태 분석
Seongsik Park, Soo-Dong Yoh, Duk-Young Chung

박성식, 여수동, 정덕영
3-phenyl-5,5-dimethyloxazolidine-2,4-dione에 대한 형태 분석을 통하여 구조-활성 관계를 검토하였다. Antifungal Activity에 대한 구조적인 특징으로 활성기인 amide group(-NCO)와 벤젠 moiety가 존재하며, 강한 활성을 나타내는 유사체의 N원자와 para 치환기 간의 공간거리 N-X4는 5.32∼5.37Å, 3,5-치환기 간의 거리 X3-X5는 5.59 ∼ 5.77 Å을 나타내었다.

The relationship between chemical structure and antifungal activity of benzene ring substituents of 3-phenyl-5,5-dimethyloxazolidine-2,4-diones is studied by testing of model compounds and use of conformational data. The analysis revealed a number of structural features as essential for the antifungal effect: (1) the presence of an intact -NCO group and benzene moiety; (2) the distance between para substituents and the N atom within the 5.32∼5.37Å range; (3) the distance between substituent X3 and X4, in the interval 5.59 ∼ 5.77 Å for the active analogues.

476 - 482
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